Emesis or vomiting is a common symptom of a variety of gastrointestinal or central nervous system disorders. Therapy is generally oriented at removing the offending stimulus or resolving the condition responsible for the vomiting. Emesis is often, but not always, accompanied by nausea, an unpleasant subjective gastrointestinal sensation which provokes the feeling that one has to vomit. Pharmacological or medicinal remedies for nausea and vomiting are few and of limited usefulness, and include the phenothiazine tranquilizers and some antihistamines effective in motion sickness.
Over the last few years, I have been engaged in utilizing the narcotic antagonist naloxone (N-allylnoroxymorphone) in the treatment of itching, see U.S. Pat. No. 4,181,726 issued to me Jan. 1, 1980. Several of the patients I have treated for chronic itching had accompanying malignancies for which they were receiving systemic cancer chemotherapy. During each course of chemotherapy these patients would all experience extreme nausea and vomiting shortly after receiving intravenous chemotherapeutic agents.
Surprising, after I placed them on the naloxone for itching, they noted marked reduction in the nausea and vomiting associated with their chemotherapeutic treatment. Then I administered naloxone intravenously, subcutaneously, intramuscularly and orally to patients prior to receiving dicarbazine or adriamycin or methotrexate for treatment of malignant melanoma. The naloxone was given 10 minutes to 1 hour before intravenous dicarbazine, adriamycin or methotrexate was administered. Each patient had markedly reduced nausea and vomiting associated with the chemotherapy and two patients who had always become very nauseous and vomited many times before with dicarbazine had no nausea or vomiting after pretreatment with naloxone. Subsequently, I administered naloxone to several patients who had nausea and vomiting associated with a viral or bacterial gastroenteritis. The naloxone partially or completely relieved the nausea and vomiting of those patients.
Furthermore, I have found that naloxone administered intravenously, subcutaneously, or intramuscularly in total daily dosages of 0.4 to 20.0 mgs administered as a single dose or divided doses ranging from 0.4 mg. to 10 mg. 2-6 times daily, or oral administration of n-methyl cyclopropyl naloxone (naltrexone) administered in divided oral dosages of from 10 to 50 mg. up to 200 mg. daily, can prevent nausea or vomiting secondary to high dose oral antibiotic therapy or secondary to acute alcohol ingestion.
Naloxone is a narcotic antagonist which is not known to cause physical or psychological dependence and which exhibits essentially no pharmacological activity in non-addicts. Naloxone is normally given by injection to addicts to assist them in narcotic withdrawal and sometimes is administered to post operative patients for partial removal of narcotic depression following the use of narcotics during surgery. Surprisingly, it has been found that naloxone or a pharmaceutically acceptable salt thereof or a chemically similar narcotic antagonist such as the n-methyl cyclopropyl derivative are useful in the prophylaxis or treatment of nausea and/or emesis.